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US 6,207,404 B1Granted
Coumarin-based CYP3A fluorescent assay reagents
AssigneeGentest Corporation
InventorsVaughn P. Miller, Charles L. Crespi
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Abstract
Novel fluorescent substrates of human cytochrome P450 enzymes are provided. Also provided are methods for their manufacture and use. These substrates are useful in assessing cytochrome P450 enzyme activity and in selecting compounds which inhibit cytochrome P450 enzyme activity and, in particular, for identifying potential adverse drug interactions which are mediated by inhibition of cytochrome P450 enzyme activity. The compounds are particularly useful for assessing cytochrome P450 CYP3A enzyme activity.
Claims30
A compound of the Formula I:
- (a) wherein R1 is an aryl containing an aryl ring carbon and/or an aryl ring nitrogen and the (CH2)n is coupled via a covalent bond to the aryl ring carbon or the aryl ring nitrogen;
- (b) wherein n is 0, 1, 2, or 3;
- (c) wherein R2 is selected from the group consisting of an hydrido, CN, CH3, sulfomethyl, and a haloalkyl having 1-18 carbons;
- (d) wherein R3 is selected from the group consisting of an hydrido, CN, and an aryl containing an aryl ring carbon and/or an aryl ring nitrogen, provided that R2 and R3 are not both hydrido, and wherein the aryl group is coupled directly to the coumarin ring via a covalent bond between the coumarin ring carbon and the aryl ring carbon or the aryl ring nitrogen;
- (e) wherein when R1 is phenyl and n is 1, R2 is not an hydrido when R3 is phenyl and R3 is not an hydrido when R2 is CH3;
- (f) wherein the compound is a cytochrome P450 substrate.
3 more elements
Dependencies are inferred from the claim text.